Bradley C Pearce
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Explore the profile of Bradley C Pearce including associated specialties, affiliations and a list of published articles.
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16
Citations
195
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Recent Articles
1.
Degnan A, Kumi G, Allard C, Araujo E, Johnson W, Zimmermann K, et al.
ACS Med Chem Lett
. 2021 Mar;
12(3):443-450.
PMID: 33732413
While the discovery of immune checkpoint inhibitors has led to robust, durable responses in a range of cancers, many patients do not respond to currently available therapeutics. Therefore, an urgent...
2.
Wang T, Ueda Y, Zhang Z, Yin Z, Matiskella J, Pearce B, et al.
J Med Chem
. 2018 Jun;
61(14):6308-6327.
PMID: 29920093
The optimization of the 4-methoxy-6-azaindole series of HIV-1 attachment inhibitors (AIs) that originated with 1 to deliver temsavir (3, BMS-626529) is described. The most beneficial increases in potency and pharmacokinetic...
3.
Marcin L, Warrier J, Thangathirupathy S, Shi J, Karageorge G, Pearce B, et al.
ACS Med Chem Lett
. 2018 May;
9(5):472-477.
PMID: 29795762
There is a significant unmet medical need for more efficacious and rapidly acting antidepressants. Toward this end, negative allosteric modulators of the -methyl-d-aspartate receptor subtype GluN2B have demonstrated encouraging therapeutic...
4.
Higgins M, Marcin L, Zusi F, Gentles R, Ding M, Pearce B, et al.
Bioorg Med Chem
. 2016 Dec;
25(2):496-513.
PMID: 27914948
Triazolopyridine ethers with mGlu positive allosteric modulator (PAM) activity are disclosed. The synthesis, in vitro activity, and metabolic stability data for a series of analogs is provided. The effort resulted...
5.
Appiah K, Blat Y, Robertson B, Pearce B, Pedicord D, Gentles R, et al.
J Biomol Screen
. 2013 Nov;
19(4):595-605.
PMID: 24241710
Recent genetic evidence suggests that the diacylglycerol lipase (DAGL-α) isoform is the major biosynthetic enzyme for the most abundant endocannabinoid, 2-arachidonoyl-glycerol (2-AG), in the central nervous system. Revelation of its...
6.
Laurent D, Serrano-Wu M, Belema M, Ding M, Fang H, Gao M, et al.
J Med Chem
. 2013 Apr;
57(5):1976-94.
PMID: 23573957
A series of symmetrical E-stilbene prolinamides that originated from the library-synthesized lead 3 was studied with respect to HCV genotype 1a (G-1a) and genotype 1b (G-1b) replicon inhibition and selectivity...
7.
Gerritz S, Cianci C, Kim S, Pearce B, Deminie C, Discotto L, et al.
Proc Natl Acad Sci U S A
. 2011 Sep;
108(37):15366-71.
PMID: 21896751
Influenza nucleoprotein (NP) plays multiple roles in the virus life cycle, including an essential function in viral replication as an integral component of the ribonucleoprotein complex, associating with viral RNA...
8.
Pedicord D, Flynn M, Fanslau C, Miranda M, Hunihan L, Robertson B, et al.
Biochem Biophys Res Commun
. 2011 Jul;
411(4):809-14.
PMID: 21787747
Diacylglycerol lipase α is the key enzyme in the formation of the most prevalent endocannabinoid, 2-arachidonoylglycerol in the brain. In this study we identified the catalytic triad of diacylglycerol lipase...
9.
Meanwell N, Wallace O, Wang H, Deshpande M, Pearce B, Trehan A, et al.
Bioorg Med Chem Lett
. 2009 Jul;
19(17):5136-9.
PMID: 19632112
1-(4-Benzoylpiperazin-1-yl)-2-(1H-indol-3-yl)ethane-1,2-dione (1a) has been characterized as an inhibitor of HIV-1 attachment that interferes with the interaction of viral gp120 with the host cell receptor CD4. In previous studies, the effect...
10.
Pearce B, Langley D, Kang J, Huang H, Kulkarni A
J Chem Inf Model
. 2009 Jun;
49(7):1797-809.
PMID: 19552372
An automated E-Novo protocol designed as a structure-based lead optimization tool was prepared through Pipeline Pilot with existing CHARMm components in Discovery Studio. A scaffold core having 3D binding coordinates...